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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Transferrin-appended PEGylated nanoparticles for temozolomide delivery to brain: in vitro characterisation
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Transferrin-appended PEGylated nanoparticles for temozolomide delivery to brain: in vitro characterisation

机译:转铁蛋白附加的聚乙二醇化纳米颗粒用于替莫唑胺递送至大脑:体外表征

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摘要

Polymer-based nanotechnologies are proposed to be an alternative for drug administration, delivery and targeting to those of conventional formulations. The blood brain barrier is frequently a rate-limiting factor in determining permeation of a drug into brain. In this study, the surface-engineered long-circulating PLGA nanoparticles (NPs) were assessed for brain-specific delivery. Long circulating NPs of PLGA- and PEG-synthesised copolymer were prepared by emulsification solvent evaporation method. Further, the surface of PEGylated NPs was modified by anchoring transferrin (Tf) ligand for receptor-mediated targeting to brain. NPs were characterised for shape and size, zeta potential, entrapment efficiency and in vitro drug release. In vitro cytotoxicity studies were performed on human cancer ceil lines. Confocal Laser Scanning Microscopy studies show the enhanced uptake of Tf-appended PEGylated NPs and their localisation in the brain tissues. Hence, the specific role of Tf ligand on PEGylated NPs for brain delivery was confirmed.
机译:提出基于聚合物的纳米技术可以替代传统配方的药物给药,递送和靶向。血脑屏障通常是确定药物向大脑渗透的速率限制因素。在这项研究中,对表面工程化的长循环PLGA纳米颗粒(NPs)进行了脑特异性递送评估。采用乳化溶剂蒸发法制备了PLGA-PEG合成的长循环NPs。此外,通过锚定转铁蛋白(Tf)配体修饰PEG化NPs的表面,以受体介导的靶向脑。对NP的形状和大小,ζ电势,包封效率和体外药物释放进行了表征。对人癌细胞株进行了体外细胞毒性研究。共聚焦激光扫描显微镜研究表明,Tf附加的PEG化NP的摄取增加,并且在脑组织中的定位也有所提高。因此,证实了Tf配体在聚乙二醇化的NPs上对于脑部递送的特异性作用。

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